Target Identification and Mechanistic Characterization of Indole Terpenoid Mimics: Proper Spindle Microtubule Assembly Is Essential for Cdh1-Mediated Proteolysis of CENP-A.

Centromere protein A (CENP-A), a histone H3 variant specific to centromeres, is crucial for kinetochore positioning and chromosome segregation. However, its regulatory mechanism in human cells remains incompletely understood. A structure-activity relationship (SAR) study of the cell-cycle-arresting indole terpenoid mimic JP18 leads to the discovery of two more potent analogs, (+)-6-Br-JP18 and (+)-6-Cl-JP18. Tubulin is identified as a potential cellular target of these halogenated analogs by using the drug affinity responsive target stability (DARTS) based method. X-ray crystallography analysis reveals that both molecules bind to the colchicine-binding site of ß-tubulin. Treatment of human cells with microtubule-targeting agents (MTAs), including these two compounds, results in CENP-A accumulation by destabilizing Cdh1, a co-activator of the anaphase-promoting complex/cyclosome (APC/C) E3 ubiquitin ligase. This study establishes a link between microtubule dynamics and CENP-A accumulation using small-molecule tools and highlights the role of Cdh1 in CENP-A proteolysis.

Effects of Al2O3 Nanoparticles on the Crystallization of Calcium Carbonate in Aqueous Solution.

The effects of Al2O3 nanoparticles on the precipitation behavior of CaCO3 and on the anti-scale performance of 2-phosphonobutane-1,2,4-tricarboxylic acid (PBTCA) in CaCO3 growth solution were studied by means of solution analysis, gravimetric methods, scanning electron microscopy, Fourier transform infrared spectroscopy and X-ray diffraction. The results illustrate that Al2O3 nanoparticles had little effect on the concentration of calcium ions in the test solution without PBTCA, but significantly changed the form and morphology of calcium carbonate crystals, which were transformed from calcite to aragonite. As a commonly used and effective scale inhibitor, PBTCA showed good Ca2+ retention ability in the test solution, distorting the calcite crystal lattice and promoting the formation of vaterite. When Al2O3 nanoparticles co-existed with PBTCA in the test solution, calcium carbonate was more likely to precipitate, and the Ca2+ retention ability of PBTCA reduced. A newly designed gravimetric method was used to evaluate the scale inhibition performance of Al2O3 nanoparticles on the heat exchange surface. When the concentration of Al2O3 nanoparticles reached 1 g/L, the surface scale inhibition efficiency of Al2O3 nanoparticles exceeded 80%.

Effect of Carbon Nanoparticles on the Crystallization of Calcium Carbonate in Aqueous Solution.

Nanofluids have great application prospects in industrial heat exchange systems because they can significantly improve the heat and mass transfer efficiency. However, the presence of nanoparticles in the fluid might also affect the formation and attachment of inorganic scales, such as calcium carbonate, on the heat exchange surface. The effects of carbon nanoparticles on the crystallization of calcium carbonate in aqueous solution were studied by the scale inhibition test, solution analysis, scanning electron microscopy (SEM), X-ray photoelectron spectroscopy (XPS), and Fourier transform infrared spectroscopy (FTIR). The results showed that carbon nanoparticles had an excellent surface scale inhibition performance for calcium carbonate, which could effectively prevent the adhesion of scale on the heat exchange surface. The carbon nanoparticles did not affect the solubility of calcium carbonate in water, but changed the crystal form of the precipitated calcium carbonate, making it difficult to adsorb on the heat exchange surface and achieving a surface scale inhibition effect. Carbon nanofluids effectively inhibit the adhesion of calcium carbonate to heat exchange surfaces.

Effects of TiO2 Nanofluid on the Surface State of Brass.

The surface states of brass in simulated cooling water (SCW) containing or free of sodium dodecyl benzene sulfonate (SDBS) and TiO2 nanofluid were analyzed by means of scanning electron microscope (SEM), energy spectrum analysis (EDS) and X-ray diffraction (XRD). The concentrations of Cu and Zn ions in the solution after brass immersion were analyzed using a plasma emission spectrometer. The relationship between the surface states and corrosion resistance of brass was investigated by electrochemical impedance spectroscopy (EIS). The results showed that the brass surface was mainly covered with zinc compound Zn5(OH)6(CO3)2 as corrosion product in SCW. In SCW containing SDBS, a large amount of SDBS was adsorbed on the brass surface. In TiO2 nanofluid, the brass surface was relatively bare and mainly contained cuprous oxide. There was no obvious adhesion of SDBS aggregates and no accumulation of zinc compound on brass surface in TiO2 nanofluid. TiO2 nanoparticles inhibit the adsorption of SDBS on brass surface. Solution analysis results showed that the concentrations of Cu and Zn ions in TiO2 nanofluid was obviously higher than that in SCW and SCW containing SDBS, indicating that most of corrosion products of brass dissolved into the nanofluid. The EIS results illustrated the brass electrode had a larger reaction resistance in SCW containing SDBS, indicating the good protective performance of the adsorbed SDBS film on brass surface. The reaction resistance of the brass electrode was the smallest in TiO2 nanofluid, which illustrated that TiO2 nanoparticles in solution promoted the corrosion of brass.

Influence of Al2O3 Nanoparticles on Corrosion Inhibition Performance of Benzotriazole to Brass.

The influence of Al2O3 nanoparticles on corrosion inhibition of benzotriazole (BTA) in brass/ simulated water system was studied by potentiodynamic polarization curve and electrochemical impedance spectroscopy (EIS). The results show that BTA has good corrosion inhibition effect on brass. Al2O3 nanoparticles could reduce the corrosion inhibition performance of BTA. The higher the concentration of Al2O3 nanoparticles in simulated water, the lower corrosion inhibition performance of BTA. The isothermal adsorption of BTA on brass surface in simulated water and Al2O3 nanofluids was analyzed. The results indicated that the adsorption of BTA on brass surface followed the Langmuirs' adsorption isotherm, the adsorption Gibbs free energy ΔG was less than -40 kJ/mol, corresponding to chemical adsorption, in both simulated water and Al2O3 nanofluids. The -ΔG value of BTA on brass surface decreased in Al2O3 nanofluids, indicating the weakening of the BTA adsorption on the brass surface. Surface analysis of brass samples by optical microscope and X-ray diffraction confirmed the above results.

[Spectral Characteristics of Dissolved Organic Matters in Reject Water from Wastewater Treatment Plants].

Reject water generated from sludge thickening, dewatering and stabilization process contains high-content and complex dissolved organic matters (DOM). The spectral characteristics of DOM in the reject water were investigated by three-dimensional excitation-emission matrix and Fourier transform infrared spectroscopy. Fluorescent DOM (FDOM) from reject water were decomposed into six components by parallel factor analysis, the protein-like C1 (275/355 nm), C4 (235/350 nm) and C6 (275/305 nm) and the humic-like C2 (250, 340/440 nm) , C3 (320/380 nm) and CS (250/465 nm). Soluble COD in the sludge thickening reject water was positively correlated with all the three humic-like substances at P < 0.01 level, and was insignificantly influenced by protein-like substances. The tryptophan-like C1, C4 and humic-like CS increased in the centrifugal dewatering reject water (CDRW). FDOM in the advanced dewatering reject water (ADRW) were significantly different from those of other reject water in fluorescence peak locations and intensities, and humic-like C3 and tyrosine-like C6 in the DOM were 15.63 and 7.30 times higher than those in CDRW. Compared to sludge thickening reject water, infrared peaks related to polysaccharide and humic substances in CDRW were enhanced and massive proteins were released into ADRW. DOM structures in ADRW were changed owing to the complexation between metals and both humic substances and proteins.

A Versatile Anisometric Metallic Supercrystal with Controllable Orientation on a Chip as a Stable and Reliable Label-Free Biosensor.

Based on anisometric noble-metal nanocrystals, a universal fabrication protocol for preparing 3D supercrystals with controlled orientation on a chip has been developed. A comparison of the surface-enhanced Raman scattering (SERS) behavior of 3D nanorod supercrystals aligned vertically and parallel to the chip indicates that the SERS-enhancing ability and reproducibility of the former is superior to the latter. The 3D nanorod supercrystals aligned vertically to the chip have been utilized as highly sensitive SERS substrates for the label-free discrimination of Gram-positive and -negative bacteria. Furthermore, to strengthen the stability of the supercrystal substrate for assays of bacteria in biosamples, a coating of the antibiotic vancomycin can dramatically increase adhesion of bacteria on a nanointerface and simultaneously improve the SERS response of bacteria to achieve a layer-by-layer assembled, stable, and reliable biosensor for bacteria.

Crystallization and preliminary crystallographic analysis of recombinant VSP1 from Arabidopsis thaliana.

VSP1 is a defence protein in Arabidopsis thaliana that may also be involved in control of plant development. The recombinant protein has been overexpressed in Escherichia coli, purified and crystallized using the sitting-drop vapour-diffusion method. The crystal diffracted to 1.9 A resolution and a complete X-ray data set was collected at 100 K using Cu Kalpha radiation from a rotating-anode X-ray source. The crystals belonged to space group C2. As there are no related structures that could be used as a search model for molecular replacement, work is in progress on experimental phasing using heavy-atom derivatives and selenomethionine derivatives.